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Assay Detail

CHEMBL5388966

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Autocuration

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.
Lucena-Agell D, Guillén MJ, Matesanz R, Álvarez-Bernad B, Hortigüela R, Avilés P, Martínez-Díez M, Santamaría-Núñez G, Contreras J, Plaza-Menacho I, Giménez-Abián JF, Oliva MA, Cuevas C, Díaz JF.
J Med Chem (2024) 67 : 2619 -2630
PubMed 38294341 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.74 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292702 MAYTANSINE 2.0 1 9.48
CHEMBL159 VINBLASTINE 4.0 1 9.27
CHEMBL92 DOCETAXEL ANHYDROUS 4.0 1 9.15
CHEMBL428647 PACLITAXEL 4.0 1 8.96
CHEMBL5437532 1 8.80
CHEMBL61 PODOFILOX 4.0 1 7.81
CHEMBL5418923 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292702 MAYTANSINE IC50 = 0.33 nM 9.48
CHEMBL159 VINBLASTINE IC50 = 0.54 nM 9.27
CHEMBL92 DOCETAXEL ANHYDROUS IC50 = 0.7 nM 9.15
CHEMBL428647 PACLITAXEL IC50 = 1.1 nM 8.96
CHEMBL5437532 IC50 = 1.6 nM 8.80
CHEMBL61 PODOFILOX IC50 = 15.5 nM 7.81
CHEMBL5418923 IC50 = 19.0 nM 7.72